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壳聚糖作为药用辅料在药剂领域中的地位愈加显著 ,将聚 β1→ 4D-葡萄糖胺的 2位氨基进行修饰 ,可获得具不同功能的壳聚糖类衍生物。对于口服氨基酸系统来说 ,最主要的是克服胃肠道的吸收屏障及酶屏障 ,未经化学修饰的壳聚糖对肽类药物具一定的促渗作用 ,将抑制剂固定于聚合物结构内则对肠肽酶对肽类的降解产生保护作用。胰丝氨酸蛋白酶的降解作用可被竞争性抑制剂如Bowman- Birk抑制剂所抑制 ,而金属肽酶的降解作用则可被壳聚糖 - EDTA复合物等性质较复杂的壳聚糖衍生物所抑制。而且 ,由于壳聚糖及其大部分衍生物都具有粘膜粘附特性 ,多肽药物的吸收前代谢也大大降低。综合以上因素 ,壳聚糖及其衍生物可显著提高某些肽类药物如胰岛素、降钙素及布舍瑞林口服给药的生物利用度 ,是肽类口服给药系统中的一类重要辅料。
As a pharmaceutical excipient, chitosan has become more and more prominent in the pharmaceutical field. Chitosan derivatives with different functions can be obtained by modifying the 2-amino group of poly-β1 → 4D-glucosamine. For oral amino acid system, the most important is to overcome the gastrointestinal absorption barrier and enzyme barrier, unmodified chitosan peptide drugs have a certain role in promoting seepage, the inhibitor is fixed in the polymer structure The protective effect of enteropeptidase on the degradation of peptides. Degradation of pancreatic serine proteases can be inhibited by competitive inhibitors such as Bowman-Birk inhibitors, whereas the degradation of metallopeptidases can be inhibited by more complex chitosan derivatives such as chitosan-EDTA complexes . Moreover, since the chitosan and most of its derivatives have mucoadhesive properties, the pre-absorption metabolism of polypeptide drugs is also greatly reduced. Based on the above factors, chitosan and its derivatives can significantly improve the bioavailability of certain peptide drugs such as insulin, calcitonin and buserelin for oral administration, which is an important class of oral delivery systems for peptides Accessories.